An efficient asymmetric vinylogous aldol/lactonization cascade reaction between β,γ-unsaturated amides and trifluoromethyl ketones has been developed. With chiral cyclohexanediamine-based tertiary amine-thiourea catalyst C4, optically active trifluoromethyl dihydropyranones have been constructed...

No abstract

A copper-catalyzed oxidative carboamination of maleimides with alkyl amines and α-bromo carboxylates is described. These multicomponent reactions show good functional group compatibility and are suitable for the late-stage modification of a series of neuroprotective agents, providing a direct path for the library synthesis of 3-carbo-4-amino maleimides. The initial copper-catalyzed oxidative amination of maleimides with amines to form enamines intermediate, followed by copper-catalyzed radical alkylation with α-bromo carboxylate compounds, triggers a relayed catalytic reaction to achieve the carboamination process.

An unprecedented copper-catalyzed oxidative aminohalogenation of electron-deficient maleimides with secondary amines and NXS (X = Cl, Br, I) was developed, in which the N−X bonds generated in situ were used as difunctionalized reagents. The distinctive features of this multicomponent reaction include a simple green catalytic system, a spectral substrate range, and the late-stage modification of drug molecules. Most importantly, this umpolung radical cascade strategy exploits the in situ formation of Niodoamines that enable efficient alkene aminoiodination.

Amine hydrochloride salts have been typically used as amination reagents. Contrary to conventional use, HCl is released as waste residue. Herein, we disclose a new utilization of amine hydrochloride as...